Abstract: The subject matter generally relates to compounds and methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.
Type:
Application
Filed:
November 9, 2018
Publication date:
May 16, 2019
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng LI, Hailin ZHENG, Jun ZHAO, Lawrence WENNOGLE
Abstract: The invention relates to the combination of inhibitors of phosphodiesterase 1 (PDE1) and inhibitors of Neprilysin (NEP) useful for the treatment of certain cardiovascular diseases or related disorders, e.g., hypertension, congestive heart disease, and post-myocardial infarction. In another embodiment, the invention relates to the combination of inhibitors of PDE1 and inhibitors of NEP for the treatment of diseases or disorders characterized by disruption of or damage to various cGMP/PKG mediated pathways in the cardiovascular system (e.g., in cardiac tissue or in arterial smooth muscle).
Abstract: The invention provides methods for the prophylaxis or treatment of one or more disorders associated with dementia comprising administering to a patient in need thereof, a therapeutically effective amount of (i) a 5-HT2A or 5-HT2A/D2 receptor ligand and (ii) a PDE1 inhibitor, and pharmaceutical compositions comprising (i) a 5-HT2A or 5-HT2A/D2 receptor ligand and (ii) a PDE1 inhibitor.
Abstract: The disclosure provides new, stable, pharmaceutically acceptable salt forms of 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, together with methods of making and using them, and pharmaceutical compositions comprising them.
Abstract: The disclosure provides new, stable, pharmaceutically acceptable co-crystal forms of 1-(4-fluoro-phenyl)-4-((6bR, 10aS)-3-methyl-2,3,6b,9, 10, 10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de[quinoxalin-8-yl)-butan-1-one, together with methods of making and using them, and pharmaceutical compositions comprising them.
Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the ?-opioid receptor.
Abstract: The present invention relates to a new use of phosphodiesterase 1 (PDE1) inhibitors for the treatment of psychosis, schizophrenia, schizoaffective disorder, schizophreniform disorder, psychotic disorder, delusional disorder, mania, or bipolar disorder.
Type:
Grant
Filed:
June 4, 2018
Date of Patent:
March 26, 2019
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Allen A. Fienberg, Lawrence P. Wennogle, Sharon Mates
Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D2 receptor signaling systems.
Type:
Application
Filed:
August 6, 2018
Publication date:
March 7, 2019
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng LI, Qiang ZHANG, Robert DAVIS, Lawrence P. WENNOGLE
Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines of Formula 2F, as shown below, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines, such methods comprising the preparation of a Compound of Formula 2F, as shown below and as further defined herein:
Type:
Grant
Filed:
July 26, 2017
Date of Patent:
March 5, 2019
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
John Charles Tomesch, Peng Li, Wei Yao, Qiang Zhang, James David Beard, Andrew S. Thompson, Hua Cheng, Lawrence P. Wennogle
Abstract: This invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.
Type:
Application
Filed:
August 3, 2018
Publication date:
February 28, 2019
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Sharon MATES, Peng LI, Lawrence P. WENNOGLE, Robert DAVIS
Abstract: The present invention relates to novel pyridinoxy phenylpropanamines, their pharmaceutical compositions and methods of use. In addition, the present invention relates to therapeutic methods that penetrate the blood-brain barrier and regulate the norepinephrine and serotonin transporters (“NET/SERT”).
Type:
Grant
Filed:
March 18, 2016
Date of Patent:
January 29, 2019
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng Li, Jun Zhao, Lawrence P. Wennogle
Abstract: The subject matter generally relates to methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.
Abstract: The invention relates to particular 2-((1-(2-hydroxy-2-phenylethyl)piperidin-4-yl)methyl)isoindolin-1-one analogs and pro-drugs, in free, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases that can be therapeutically and/or preventively treated by the nerve control function of sigma ligands.
Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.
Type:
Application
Filed:
September 7, 2018
Publication date:
January 3, 2019
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng LI, Hailin ZHENG, Gretchen SNYDER, Lawrence P. WENNOGLE, Joseph HENDRICK
Abstract: The subject matter generally relates to compounds and methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.
Type:
Grant
Filed:
September 17, 2015
Date of Patent:
December 11, 2018
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng Li, Hailin Zheng, Jun Zhao, Lawrence Wennogle
Abstract: The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.
Type:
Grant
Filed:
August 7, 2015
Date of Patent:
November 20, 2018
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.
Type:
Grant
Filed:
March 23, 2017
Date of Patent:
November 6, 2018
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Sharon Mates, Allen Fienberg, Lawrence P. Wennogle
Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.
Type:
Grant
Filed:
December 7, 2015
Date of Patent:
October 23, 2018
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng Li, Hailin Zheng, Gretchen Snyder, Lawrence P. Wennogle, Joseph Hendrick
Abstract: The present invention relates to a new use of phosphodiesterase 1 (PDE1) inhibitors for the treatment of psychosis, schizophrenia, schizoaffective disorder, schizophreniform disorder, psychotic disorder, delusional disorder, mania, or bipolar disorder.
Type:
Application
Filed:
June 4, 2018
Publication date:
October 4, 2018
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Allen A. FIENBERG, Lawrence P. WENNOGLE, Sharon MATES
Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.
Type:
Grant
Filed:
April 3, 2015
Date of Patent:
September 18, 2018
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Sharon Mates, Peng Li, Lawrence P. Wennogle, Robert Davis